Daclatasvir Dihydrochloride
API’s Name：Daclatasvir Dihydrochloride
CAS No.：1009119-65-6
Indication：HCV
Innovator：
Specification：In-House
US DMF：√
EU DMF：
CEP：
Only for R&D purpose
Intermediates
Product Detail
Description
Daclatasvir dihydrochloride (BMS-790052 dihydrochloride) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir dihydrochloride is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 µM and 3.27 µM, respectively.
IC50 & Target
EC50: 50 pM (HCV replicon genotype 1a), 9 pM (HCV replicon genotype 1b), 71 pM (HCV replicon genotype 2a), 146 pM (HCV replicon genotype 3a), 12 pM (HCV replicon genotype 4a) and 33 pM (HCV replicon genotype 5a)[1]
Kd: 8 nM (NS5A33-202) and 210 nM (NS5A26-202)[2]
IC50: 1.5 µM (OATP1B) and 3.27 µM (OATP1B3)[3]
In Vitro
Daclatasvir (BMS-790052) demonstrates potent inhibitory activity towards all genotypes tested, with EC50 values ranging from 9 pM to 146 pM. Daclatasvir inhibits HCV replicon genotype 1a, 1b, 2a, 3a, 4a and 5a with EC50 values of 50 pM, 9 pM, 71 pM, 146 pM, 12 pM and 33 pM, respectively. Daclatasvir is a potent inhibitor of the JFH-1 genotype 2a infectious virus that replicates in cell culture (EC50=28 pM)[1]. Daclatasvir (BMS-790052) binds tightly to NS5A33-202 and NS5A26-202 with Kds of 8 nM and 210 nM, respectively[2].
Storage
| Powder | -20°C | 3 years |
4°C | 2 years | |
| In solvent | -80°C | 6 months |
-20°C | 1 month |
Clinical Trial
NCT Number | Sponsor | Condition | Start Date | Phase |
NCT03369327 | Tehran University of Medical Sciences|RojanPharma Pharmaceutical Company | Hepatitis C Virus Infection, Response to Therapy of|Human Immunodeficiency Virus | January 1, 2017 | Phase 3 |
NCT03485846 | R-Pharm|Almedis | Chronic Hepatitis C Genotype 1b | November 27, 2017 | Phase 2 |
NCT01016912 | Bristol-Myers Squibb | Hepatitis C Infection | December 2009 | Phase 2 |
NCT01629732 | Bristol-Myers Squibb | Hepatitis C Virus | March 2013 | Phase 2 |
NCT01497834 | Bristol-Myers Squibb | Hepatitis C | January 2012 | Phase 3 |
NCT01973049 | Bristol-Myers Squibb | Hepatitis C | December 2013 | Phase 3 |
NCT00663208 | Bristol-Myers Squibb | Chronic Hepatitis C | May 2008 | Phase 2 |
NCT02576314 | Humanity and Health Research Centre|Beijing 302 Hospital | Chronic Hepatitis C Infection | May 2015 | Phase 3 |
NCT02756936 | Genuine Research Center, Egypt|Zeta Pharma Pharmaceutical Industries | Healthy | February 2016 | Phase 1 |
NCT02771405 | National Hepatology & Tropical Medicine Research Institute|Cairo University | Hepatitis C, Chronic|Hepatocellular Carcinoma | March 2016 | Phase 3 |
NCT03706898 | Viriom | HIV-1-infection|Hepatic Impairment | October 1, 2018 | Phase 1 |
NCT02319031 | Bristol-Myers Squibb | Hepatitis C | February 2015 | Phase 3 |
NCT02124044 | National Institutes of Health Clinical Center (CC)|National Institute of Allergy and Infectious Diseases (NIAID)|Bristol-Myers Squibb | HIV-HCV | February 2014 | Phase 2 |
NCT02551861 | Bristol-Myers Squibb | Hepatitis C | December 2015 | Phase 2 |
NCT00859053 | Bristol-Myers Squibb | Hepatic Insufficiency | March 2009 | Phase 1 |
NCT01257204 | Bristol-Myers Squibb | Hepatitis C Virus | December 2010 | Phase 2 |
NCT03063879 | Tehran University of Medical Sciences|Ahvaz Jundishapur University of Medical Sciences|Shiraz University of Medical Sciences|Hamadan University of Medical Science | Hepatitis C, Chronic|Chronic Renal Failure | April 1, 2017 | Phase 4 |
NCT01017575 | Bristol-Myers Squibb | Hepatitis C Infection | December 2009 | Phase 2 |
NCT02865369 | Sang Gyune Kim|Seoul National University Boramae Hospital|Severance Hospital|Inha University Hospital|Korea University|Gachon University Gil Medical Center|Hanyang University Seoul Hospital|Ewha Womans University Mokdong Hospital|Bristol-Myers Squibb|Soonchunhyang University Hospital | Chronic Hepatitis C | September 2016 | |
NCT04070235 | Nanjing Sanhome Pharmaceutical, Co., Ltd. | Hepatitis C, Chronic | March 29, 2019 | Phase 2|Phase 3 |
NCT03487848 | Bristol-Myers Squibb | Hepatitis C|Chronic Hepatitis | May 18, 2018 | Phase 2 |
NCT00904059 | Bristol-Myers Squibb | Hepatitis C | May 2009 | Phase 1 |
NCT02107365 | French National Institute for Health and Medical Research-French National Agency for Research on AIDS and Viral Hepatitis (Inserm-ANRS)|Bristol-Myers Squibb | Hepatitis C Virus Genotype 4 Infection | November 2013 | Phase 2 |
NCT02397395 | Janssen R&D Ireland | Renal Impairment|End-stage Renal Disease | May 2015 | Phase 2 |
NCT03169348 | Assiut University | Hepatitis C | November 1, 2017 | Not Applicable |
NCT02323594 | Bristol-Myers Squibb | Hepatitis C Infection | December 2014 | Phase 1 |
NCT03537196 | French National Institute for Health and Medical Research-French National Agency for Research on AIDS and Viral Hepatitis (Inserm-ANRS) | Hepatitis C|Drug Use|Viral Hepatitis C | November 13, 2018 | Phase 4 |
NCT02103569 | Bristol-Myers Squibb | Hepatitis C | April 2014 | Phase 1 |
NCT02772744 | Zagazig University|Cairo University | Hepatitis C | November 1, 2017 | |
NCT01718158 | Bristol-Myers Squibb | Hepatitis C | January 2013 | Phase 3 |
NCT02496078 | Bristol-Myers Squibb | Hepatitis C | August 2015 | Phase 3 |
NCT01425970 | Bristol-Myers Squibb | Hepatitis C | May 2012 | Phase 2 |
NCT01471574 | Bristol-Myers Squibb | Hepatitis C, Genotype 1 | December 2011 | Phase 3 |
NCT01573351 | Bristol-Myers Squibb | Hepatitis C Virus | May 2012 | Phase 3 |
NCT01938625 | Janssen R&D Ireland | Hepatitis C, Chronic | December 12, 2013 | Phase 2 |
NCT01492426 | Bristol-Myers Squibb | Hepatitis C | January 2012 | Phase 3 |
NCT03480932 | Johns Hopkins Bloomberg School of Public Health|National Institute on Drug Abuse (NIDA)|YR Gaitonde Centre for AIDS Research and Education | Hepatitis C, Chronic | February 2, 2018 | Phase 2|Phase 3 |
NCT03163849 | Assiut University | Chronic Hepatitis c | September 1, 2019 | Phase 3 |
NCT01581203 | Bristol-Myers Squibb | Hepatitis C Virus | May 2012 | Phase 3 |
NCT01492504 | Bristol-Myers Squibb | Hepatitis C | February 7, 2012 | |
NCT03686722 | Mohamed Raslan|Ain Shams University|Drug Research Centre, Cairo, Egypt | Diabetes Mellitus, Type 2|Hepatitis C|Drug Interactions | September 9, 2017 | Phase 1 |
NCT02262728 | Janssen Research & Development, LLC | Hepatitis C, Chronic | September 30, 2014 | Phase 2 |
NCT02349048 | Janssen Research & Development, LLC | Hepatitis C Virus | January 2015 | Phase 2 |
NCT03882307 | Assiut University | Hepatitis C, Chronic | May 2020 | Early Phase 1 |
NCT02758509 | Parc de Salut Mar | Chronic Hepatitis C|Cirrhosis | January 1, 2010 | |
NCT01795911 | Bristol-Myers Squibb | Hepatitis C | March 2013 | Phase 2 |
NCT03549832 | Assiut University|Sohag University|South Valley University | HCV Coinfection | January 1, 2018 | Not Applicable |
NCT02161939 | Bristol-Myers Squibb | Chronic Hepatitis C |
| |
NCT01309932 | Bristol-Myers Squibb | Hepatitis C | March 2011 | Phase 2 |
NCT01995266 | Bristol-Myers Squibb | Hepatitis C | February 28, 2014 | Phase 3 |
NCT02640157 | AbbVie | Chronic Hepatitis C|Hepatitis C Virus|Genotype 3 Hepatitis C Virus | December 2015 | Phase 3 |
NCT02032875 | Bristol-Myers Squibb | Hepatitis C | March 2014 | Phase 3 |
NCT02624063 | Federal University of São Paulo | Hepatitis C, Chronic | December 2015 | Phase 4 |
NCT00546715 | Bristol-Myers Squibb | Chronic Hepatitis C | November 2007 | Phase 1|Phase 2 |
NCT01718145 | Bristol-Myers Squibb | Hepatitis C Virus Infection | November 2012 | Phase 3 |
NCT01616524 | Bristol-Myers Squibb | Hepatitis C Virus (HCV) | July 2012 | Phase 3 |
NCT02032901 | Bristol-Myers Squibb | Hepatitis C | January 2014 | Phase 3 |
NCT03540212 | Ain Shams University | Chronic HCV Infection | December 10, 2017 | Phase 2|Phase 3 |
NCT02097966 | Bristol-Myers Squibb | Chronic Hepatitis C |
| |
NCT02596880 | Tehran University of Medical Sciences | Hepatitis C|Cirrhosis | September 2015 | Phase 3 |
NCT04019717 | Atea Pharmaceuticals, Inc. | Hepatitis C|Hepatitis C, Chronic|Chronic Hepatitis C|Hepatitis C Virus Infection|HCV Infection | June 20, 2019 | Phase 2 |
NCT02992457 | Tanta University | Hepatitis C | January 2015 | Phase 4 |
NCT03547895 | Zagazig University | Decompensated Cirrhosis | June 1, 2015 | Not Applicable |
NCT03004625 | Kaohsiung Medical University Chung-Ho Memorial Hospital|Chang Gung Memorial Hospital|National Taiwan University Hospital|Taipei Veterans General Hospital, Taiwan|China Medical University Hospital|National Cheng-Kung University Hospital | Hepatitis C | November 2016 | Phase 3 |
NCT01051414 | Bristol-Myers Squibb | Hepatitis C Infection | April 2010 | Phase 2 |
NCT02309450 | French National Institute for Health and Medical Research-French National Agency for Research on AIDS and Viral Hepatitis (Inserm-ANRS)|Bristol-Myers Squibb | Hepatitis C Virus Genotype 4 Infection | December 2014 | Phase 2 |
NCT01628692 | Bristol-Myers Squibb|Janssen Research & Development, LLC | Hepatitis C Virus | July 2012 | Phase 2 |
NCT03186313 | Egyptian Liver Hospital|Wadi El Nil Hospital | Hepatitis C | September 2016 | Phase 3 |
NCT03063723 | Third Affiliated Hospital, Sun Yat-Sen University | Chronic Hepatitis C (Disorder) | January 1, 2016 | |
NCT00983957 | Bristol-Myers Squibb | Chronic Hepatitis C | October 2009 | Phase 1 |
NCT01725542 | French National Institute for Health and Medical Research-French National Agency for Research on AIDS and Viral Hepatitis (Inserm-ANRS)|Bristol-Myers Squibb | HCV-HIV Co-Infection | December 2012 | Phase 2 |
NCT02282709 | Foundation for Liver Research | Chronic Hepatitis C | February 2014 | Phase 3 |
NCT02032888 | Bristol-Myers Squibb | Hepatitis C | February 2014 | Phase 3 |
NCT03247296 | MTI University | Hepatitis C | February 28, 2017 | |
NCT01389323 | Bristol-Myers Squibb | Hepatitis C | September 2011 | Phase 3 |
NCT02556086 | Bristol-Myers Squibb | Hepatitis C | December 2015 | Phase 2 |
NCT01741545 | Bristol-Myers Squibb | Hepatitis C Virus | March 31, 2013 | Phase 3 |
NCT01866930 | Bristol-Myers Squibb | Chronic Hepatitis C Infection | July 11, 2013 | Phase 3 |
NCT02268864 | Janssen-Cilag International NV | Hepatitis C, Chronic | January 2015 | Phase 2 |
NCT01797848 | Bristol-Myers Squibb | Hepatitis C | June 2014 | Phase 3 |
NCT03166280 | Eman Sayed Hassan Abd Allah|Assiut University | Hepatitis C | June 2017 | |
NCT02159352 | Bristol-Myers Squibb | Hepatitis C | June 2014 | Phase 1 |
NCT01125189 | Bristol-Myers Squibb | Hepatitis C Virus | July 2010 | Phase 2 |
NCT03748745 | Nanjing Sanhome Pharmaceutical, Co., Ltd. | Drug Interactions | November 19, 2018 | Phase 1 |
NCT01012895 | Bristol-Myers Squibb | Chronic Hepatitis C | December 2009 | Phase 2 |
NCT02565888 | Radboud University | Hepatitis C|HIV | November 2015 | Phase 1 |
NCT02555943 | Humanity and Health Research Centre|Beijing 302 Hospital|Nanfang Hospital of Southern Medical University | Chronic Hepatitis C Infection|HBV Coinfection|Hepatitis B Reactivation | February 2015 | Phase 2|Phase 3 |
NCT02304159 | Tarek I. Hassanein, M.D., FACP, FAG, AGAF|Southern California Research Center | Hepatitis C|Cirrhosis | January 2015 | Phase 4 |
NCT02580474 | Myeong Jun Song|Bristol-Myers Squibb|Soonchunhyang University Hospital|Dankook University|Chungnam National University Hospital|Konyang University Hospital|Eulji University Hospital|Saint Vincent´s Hospital, Korea|Konkuk University Hospital|Cheongju St. Mary´s Hospital, Cheongju, Korea|Severance Hospital|Korea University Guro Hospital|Eulji General Hospital|The Catholic University of Korea | Hepatitis C | February 2016 | Phase 4 |
NCT02104843 | Bristol-Myers Squibb | Hepatitis C | April 2014 | Phase 1 |
NCT01428063 | Bristol-Myers Squibb | Hepatitis C Virus Infection | September 2011 | Phase 2 |
NCT02123654 | Bristol-Myers Squibb | Hepatitis C Virus Infection | April 2014 | Phase 3 |
NCT02565862 | Radboud University | Hepatitis C|Diabetes Mellitus|Insulin Resistance | January 2016 | Phase 1 |
NCT04211844 | Ain Shams University | Chronic Hepatitis C | October 1, 2019 | |
NCT00874770 | Bristol-Myers Squibb | Hepatitis C Infection | June 2009 | Phase 2 |
NCT03883698 | Sanjay Gandhi Postgraduate Institute of Medical Sciences | Kidney Failure, Chronic|Hepatitis C | March 15, 2019 | Phase 3 |
NCT01448044 | Bristol-Myers Squibb | Hepatitis C | December 2011 | Phase 3 |
NCT01359644 | Bristol-Myers Squibb|Pharmasset | Chronic Hepatitis C | June 2011 | Phase 2 |
NCT01842451 | Vertex Pharmaceuticals Incorporated | Chronic Hepatitis C|CHC|HCV|Hepatitis C | June 2013 | Phase 2 |
NCT02762448 | Tainan Municipal Hospital | Hepatitis c | July 2016 | |
NCT02473211 | Humanity and Health Research Centre|Beijing 302 Hospital | Chronic Hepatitis C Infection | January 2015 | Phase 2|Phase 3 |
NCT01455090 | Bristol-Myers Squibb | Chronic Hepatitis C | November 30, 2011 | Phase 2 |
NCT03490097 | Ain Shams University | Chronic Hepatitis c|Metabolic Syndrome | December 1, 2017 | Phase 2|Phase 3 |
NCT01170962 | Bristol-Myers Squibb | Hepatitis C Virus | August 2010 | Phase 2 |
NCT02333292 | Valme University Hospital|Hospital del SAS de Jerez|Hospital General Universitario Elche|Hospital La Línea de la Concepción|Complexo Hospitalario Universitario de A Coruña|Hospital de Figueres|Hospital Universitario Puerto Real|Hospital Universitario Virgen de la Victoria|Hospital Universitario de Canarias|Hospital General Universitario de Alicante|Hospital Universitario Araba|Hospital Royo Vilanova|Hospital Universitario de Burgos|Complejo Hospitalario Universitario de Huelva|Hospital Universitario Reina Sofia de Cordoba|Hospital Universitario Virgen Macarena|Complexo Hospitalario Universitario de Vigo|Clinica Universidad de Navarra, Universidad de Navarra|Hospital Clinico Universitario San Cecilio|Hospital Universitario La Fe|Hospital General Universitario de Valencia|Hospital Universitario Infanta Leonor|Hospital Universitario de Gran Canaria|Hospital General Universitario Santa Lucía|Centro Penitenciario Alicante 1|Hospital Regional Universitario Carlos Haya|Hospital Virgen de la Luz|Hospital General Universitario de Castellón|Hospital Parc Taulí, Sabadell | Chronic Hepatitis C Infection | December 2014 | |
NCT03200184 | Tehran University of Medical Sciences | Hepatitis C | September 1, 2016 | Phase 4 |
NCT03188276 | Third Affiliated Hospital, Sun Yat-Sen University | Chronic Hepatitis C | February 1, 2016 | Early Phase 1 |
NCT01830205 | Bristol-Myers Squibb | Hepatitis C | September 2012 | Phase 1 |